Organisch-Chemisches Institut, Int. NRW Graduate School of Chemistry, Westfälische Wilhelms-Universität Münster, Corrensstrasse 40, 48149 Münster, Germany.
J Am Chem Soc. 2013 Jun 19;135(24):8802-5. doi: 10.1021/ja4033555. Epub 2013 Jun 7.
Substituted 1H-indazoles can be formed from readily available arylimidates and organo azides by Rh(III)-catalyzed C-H activation/C-N bond formation and Cu-catalyzed N-N bond formation. For the first time the N-H-imidates are demonstrated to be good directing groups in C-H activation, also capable of undergoing intramolecular N-N bond formation. The process is scalable and green, with O2 as the terminal oxidant and N2 and H2O formed as byproducts. Moreover, the products could be transformed to diverse important derivatives.
取代的 1H-吲唑可以通过 Rh(III)-催化的 C-H 活化/C-N 键形成和 Cu-催化的 N-N 键形成，由易得的芳基异氰酸酯和有机叠氮化物形成。首次证明 N-H-异氰酸酯是 C-H 活化中良好的导向基团，也能够进行分子内 N-N 键形成。该过程可规模化进行且绿色环保，以 O2 作为末端氧化剂，生成 N2 和 H2O 作为副产物。此外，产物可以转化为多种重要的衍生物。
